KR20180062763A - Composition for anti-inflammatory - Google Patents

Abstract

The present invention relates to an anti-inflammatory composition. According to the present invention, the composition has excellent skin stability and is not only harmless to human body, but also has an excellent anti-inflammatory effect by controlling an expression of an inflammatory skin disease related mediator, and thus can be used as an anti-inflammatory composition. The composition comprises glyceryl glucoside and hyaluronic acid as active ingredients.

Description

COMPOSITION FOR ANTI-INFLAMMATORY [0002]

The present invention relates to an anti-inflammatory composition which is free of toxicity and effectively inhibits the expression of an inflammatory skin disease-related mediator and has an elevated anti-inflammatory activity.

Skin inflammation is caused by damage or destruction of cells or tissues due to external biologic causes (bacteria, viruses, parasites), physical causes (mechanical stimulation, heat, radiation, electricity) , A localized immune response that minimizes the damage and restores the damaged site to its original state.

The inflammatory reaction is a useful defense mechanism to protect the living body and to remove the products produced by the tissue damage. Various inflammatory mediators and immune cells that are present in the local blood vessels and body fluids are related to the enzyme activation, inflammatory mediator secretion, , Cell migration, tissue destruction, erythema, edema, fever or pain, or may cause dysfunction due to such symptoms.

These inflammatory reactions are involved in various biochemical phenomena, and in particular, the reactions are initiated or controlled by various enzymes involved in the inflammatory response produced by immune cells. Specifically, the immune cells migrate to the injured region via blood vessels with the help of histamine, nitric oxide (NO) or prostaglandin E2 (PGE2), and initiate an inflammatory reaction. The immune cells migrated to the injured site are cytokines such as TNF-alpha, IL-1 beta (interleukin-1 beta) or IL-6 (interleukin-6) -8 or MCP-1 to kill direct external invasive substances or collect other immune cells to initiate an inflammatory response.

Expression of iNOS (inducible nitric oxide synthase) and COX-2 (cyclooxygenase-2) when exposed to inflammation-inducing substances such as interferon-γ, lipoteichoic acid and lipopolysaccharide (LPS) And NO and PGE2 are excessively produced. These inflammatory initiators (iNOS, COX-2, TNF-α, IL-6, etc.) promote transcription by activated NF-κB, and if NO is produced unnecessarily, Tissue damage caused by inflammatory reactions, mutagenesis, damage to nerve tissue, or even chronic inflammation leading to more severe tissue damage.

Currently, synthetic medicines such as ibuprofen, antihistamines, steroids, cortisone, immunosuppressants, and immunosuppressive agents are used for the prevention and treatment of inflammatory skin diseases, but the therapeutic effect is temporary, simple symptom relief, hypersensitivity reaction, And there was a limit to the fundamental treatment of inflammation. In addition, Patent Literatures 1 to 4 disclose various attempts to develop a cosmetic composition having a anti-inflammatory function using a natural extract. However, due to other reasons such as skin irritation or discoloration, the use amount thereof is limited or the solubility in water is poor It was difficult to achieve practical effects due to limitations in application of actual products.

As a result of intensifying studies on the degree of inhibition of the inflammatory cytokine or chemokine, which is an inflammatory skin disease-related mediator, the present applicant has found that a combination of specific components known as moisturizing agents can inhibit cytokine (IL-6 etc.) and chemokine IL-8, MCP-1, etc.) as well as a remarkably synergistic effect in comparison with the case of using it as a sole component, and completed the present invention to provide a anti-inflammatory composition comprising the same.

(Patent Document 1) Korean Patent No. 0563548 (Patent Document 2) Korean Patent No. 0697319 (Patent Document 3) Korean Patent No. 1309172 (Patent Document 4) Korean Patent Registration No. 1141802

It is an object of the present invention to provide a anti-inflammatory composition that does not cause skin side effects and can effectively inhibit skin inflammation.

Another object of the present invention is to provide an anti-inflammatory composition which can provide an improved moisturizing effect with excellent skin adhesion and provide a cooling effect, thereby maximizing a skin soothing effect.

The present invention provides a anti-inflammatory composition comprising glyceryl glucoside and hyaluronic acid as an active ingredient.

The anti-inflammatory composition according to an embodiment of the present invention can regulate stimulation and inflammation by regulating cytokines and chemokines or inhibiting the expression of inflammatory mediators. In detail, the anti-inflammatory composition according to the present invention is useful as a cytokine such as interleukin-6 (IL-6), interleukin-8 (IL-8), monocyte chemotactic protein (Prostaglandin E ₂ , PGE 2), which are excessively produced by chemokines such as MCP-1 and MCP-1, and the like, thereby suppressing and blocking the inflammatory reaction.

According to one aspect of the present invention, there is provided a cosmetic composition for improving inflammation.

According to one aspect of the present invention, there is provided a pharmaceutical composition for preventing and ameliorating an inflammatory skin disease.

According to the present invention, it is possible to inhibit and block the inflammatory reaction by inhibiting the activity of inflammation mediator molecules, such as nitrogen monoxide, prostaglandin (prostaglandin E ₂ , PGE 2), as well as the regulation of cytokines. In particular, the present invention effectively inhibits inflammation-related cytokines (such as IL-6) and chemokines (such as IL-8 and MCP-1) in macrophages and inhibits the formation of NO secreted by macrophages after LPS stimulation , And has an excellent anti-inflammatory effect.

Furthermore, the anti-inflammatory composition according to the present invention does not cause toxicity or side effects, and thus can be safely applied to various cosmetic formulations and pharmaceutical compositions.

The anti-inflammatory composition according to the present invention will be described in detail below. Unless otherwise defined, technical terms and scientific terms used herein have the same meaning as commonly understood by those skilled in the art. The description of known functions and configurations that may unnecessarily obscure the gist of the present invention will be omitted.

As used herein, the term "inflammation " refers to a phenomenon that occurs when a cell or tissue is damaged due to any cause, for the purpose of minimizing the reaction and restoring the damaged part to the original state, Which causes pain, swelling, redness, fever, and the like, resulting in dysfunction, dysfunction, and dysfunction. The inflammatory skin diseases caused by inflammation are selected from the group consisting of atopic dermatitis, psoriasis, contact dermatitis, eczematous dermatitis, photodermatitis, seborrheic dermatitis, herpes dermatitis, herpes dermatitis, squamous cell, And may be at least one selected from the group consisting of inflammation, scleroderma, dermatomyositis, multiple myositis, inflammatory muscle lesions, leprosy, and three-point syndromes, and allergic dermatitis such as urticaria, insect allergies, food allergies and drug allergies Belongs.

In addition, the inflammation is caused by various biochemical phenomena in vivo. In particular, the inflammation is caused by an enzyme involved in biosynthesis of prostaglandin from arachidonic acid, such as cyclooxygenase (COX) and L-arginine Nitric oxide synthase (NOS), an enzyme that produces nitric oxide (NO) from L-arginine, is known to play an important role in mediating inflammatory responses.

The term " prostaglandin " used in the present invention is a kind of physiologically active hormone synthesized in the body and has a function of regulating the inflammatory reaction. There are three types of prostaglandins, PGE1, PGE2 and PGE3. PGE1 and PGE3, , And PGE2 induces inflammation. The prostaglandin is biosynthesized through cyclooxygenase (COX) using arachidonic acid as a precursor.

The term "cyclooxygenase (COX)" used in the present invention is an enzyme that catalyzes the first step of the synthesis of prostaglandin, wherein two molecules of oxygen are introduced into arachidonic acid to synthesize PGE2, Also called peroxides synthase. On the other hand, cyclooxygenase (COX) also has two types of isoforms, COX-1 and COX-2. It is known that COX-1 is always present in cells to synthesize prostaglandins necessary for cytoprotective action, while COX-2 is known to play an important role in inflammatory reaction by rapidly increasing in cells during inflammatory reaction.

The term "nitric oxide (NO)" in the present invention is known to be caused by various cytokines or iNOS (induced NOS) induced by external stimuli and causes cytotoxicity or various inflammatory responses . Chronic inflammation is also known to be associated with increased iNOS activity (Appleton L. et al. Pharmacol., 35. 27-28.1996).

The term "comprising as an active ingredient" used in the present invention means an anti-inflammatory composition, which means that it contains an effective amount to such an extent that it can exhibit anti-inflammatory effect.

The term "application, " as used herein, refers to contacting a composition according to the present invention to the skin of an individual by any suitable method, thereby aiming to absorb the composition into the skin.

As used herein, the term "improvement" refers to any action that improves or alters the inflammatory state by application of the composition according to the present invention.

 In the invention, " dissolution " includes not only a state of being completely dissolved in a solvent containing water but also a state of being solubilized by micelles or the like, or a state of being visually transparent and uniformly dispersed in an aqueous solvent, Which is measured by the test method.

The Applicant has deeply studied the degree of inhibition of the activity of inflammatory cytokine, an inflammatory skin disease-related mediator, and found that the combination of specific ingredients known as moisturizing agents shows anti-inflammatory effects. Further, according to the present invention, there is provided a novel anti-inflammatory composition which exhibits an unexpected superior synergistic anti-inflammatory effect according to the simple combination of each ingredient and has no irritation to the skin and can be safely used in various formulations .

An anti-inflammatory composition according to an embodiment of the present invention includes glyceryl glucoside and hyaluronic acid as an active ingredient.

The anti-inflammatory composition according to an embodiment of the present invention can inhibit the expression of proteins at various levels related to inflammation and effectively inhibit and block the secretion of NO that directly induces inflammation. In particular, the present invention effectively inhibits inflammation-related cytokines (such as IL-6) and chemokines (such as IL-8 and MCP-1) in macrophages and inhibits NO formation secreted by macrophages after LPS stimulation , Exhibiting excellent anti-inflammatory effect.

The anti-inflammatory composition according to one embodiment of the present invention has an advantage that it can provide an improved moisturizing effect and a cooling effect with excellent skin adhesion. Further, according to the present invention, since the heavy and slippery hyaluronic acid inherent feeling of use is lightly and neatly converted, it is applied to the skin with a soft feeling of use, and the excellent anti-inflammatory effect described above can be effectively delivered to the skin.

At this time, the hyaluronic acid has a chain structure in which D-glucuronic acid and N-acetyl-D-glucosamine are linked by a β-1,3 bond and alternately repeatedly connected by a β-1,4 bond. To millions of polymeric polysaccharides with very high viscosity. This can be obtained by conventional methods, for example, by extraction from the crest of a chicken or by fermentation. The hyaluronic acid according to an embodiment of the present invention also includes a salt form of hyaluronic acid. Examples of the salt of hyaluronic acid include sodium hyaluronate and potassium hyaluronate, but all pharmaceutically acceptable salt forms are also included in the present invention. At this time, the hyaluronic acid is not limited to polymer hyaluronic acid, low molecular weight hyaluronic acid and the like as long as it is used in the art. The polymer hyaluronic acid may have a weight average molecular weight of 500,000 to 3,000,000 Da, and the low molecular weight hyaluronic acid may have a weight average molecular weight of less than 500,000 Da. In order to maximize the moisturizing effect and the cooling effect, It is preferable to use a mixture of low molecular weight hyaluronic acid and high molecular weight hyaluronic acid, but it is not limited thereto.

The amount of glyceryl glucoside and hyaluronic acid to be used in the anti-inflammatory composition according to an embodiment of the present invention is not limited, but it is preferable that the glyceryl glucoside and hyaluronic acid are applied to the skin with excellent adhesiveness so as to provide skin soothing effect and maximize the desired anti- Preferably, hyaluronic acid may be contained in an amount of 10 to 200 parts by weight based on 100 parts by weight of glyceryl glucoside, and more preferably, it may include hyaluronic acid in a range of 50 to 150 parts by weight.

The anti-inflammatory composition according to an embodiment of the present invention may further include a solvent having two or more hydroxyl groups. At this time, the solvent having two or more hydroxyl groups is not limited as long as it is a conventional one, but it is preferable that the solvent is highly compatible with glyceryl glucoside and hyaluronic acid to enhance formulation stability, Preferably glycerin alone or mixed daily for containing glycerin. At this time, the solvent having two or more hydroxyl groups added to the mixed solvent containing glycerin is 1,3-propanediol, 1,3-butanediol, 1,5-pentanediol, 1,2-hexanediol, - octanediol, 1,10-decanediol, and the like. In particular, in the case of a mixed solvent in which at least one selected from the above-mentioned glycerin and 1,2-hexanediol, 1,8-octanediol and 1,10-decanediol is mixed, surprisingly, the combination of glyceryl glucoside And synergy. In addition, the anti-inflammatory composition according to an embodiment of the present invention has priority in that it can remarkably improve solubilization ability of insoluble or insoluble materials when the above-mentioned mixed solvent containing glycerin is included.

The amount of the solvent having two or more hydroxyl groups is not limited, but may be in the range of 0.5 to 20 wt%, preferably 1 to 15 wt%, more preferably 1 to 10 wt% . For example, when the solvent having two or more hydroxyl groups is used for mixing, the solvent may be added in an amount of 10 parts by weight to 200 parts by weight based on 100 parts by weight of glycerin.

In addition, the anti-inflammatory composition according to one aspect of the present invention assists in solubilizing water-insoluble or insoluble substances. At this time, a preferable example of the insoluble or insoluble substance is a flavonoid component. Most of the flavonoids have a glycoside-type structure and are known to exhibit various physiological activities such as antioxidation, anti-allergy, anti-inflammation, and antibacterial activity. However, they are representative raw materials of water insolubility or insolubility. In order to apply them as formulations, they have to be used after solubilization treatment using an excess amount of surfactant or solubilization treatment using techniques such as collection.

However, it has surprisingly been found that the anti-inflammatory composition according to one embodiment of the present invention can significantly improve the solubility of the flavonoid component. According to this, even though the conventional method for solubilizing the flavonoid component is not used, the flavonoid component can be solubilized more than an effective amount. In particular, in view of maximizing the efficacy and effect of the flavonoid component as well as a synergistic effect in the anti-inflammatory / antibacterial effect, preferred examples of the flavonoid component include apigenin, catechin, daidzein, Naringin, quercetin and the like, and their derivatives are also included in one aspect of the present invention.

For example, according to one embodiment of the present invention, it was confirmed that the solubility of catechin in the flavonoid component can be remarkably improved to 200 times or more (solubility of catechin in water, 5 μg / ml). It was also confirmed that solubilization of the flavonoid component, which was possible only in the presence of base, such as quercetin and apigenin (solubility in water, 5 mg / ml in 1 M KOH) was also possible. That is, according to the present invention, it is possible to prevent a phenomenon (for example, deterioration of discoloration, detachment, titer, etc.) caused by an excessive amount of surfactant or base used for solubilizing a flavonoid component, The effective amount and the effect can be optimally expressed. At this time, the amount of the flavonoid to be used is not limited, but when it is used in the range of 0.001 to 0.2% by weight based on the total weight of the composition, the effect is not limited to the above-mentioned effect.

The anti-inflammatory composition according to one embodiment of the present invention may be involved in the inhibition of at least one of the expression of interleukin-6, the expression of interleukin-8, and the expression of monocyte chemoattractant protein-1.

In addition, the anti-inflammatory composition according to one embodiment of the present invention can be formulated into a cosmetic composition, a pharmaceutical composition or the like.

At this time, the cosmetic composition or the pharmaceutical composition containing the anti-inflammatory composition according to one embodiment of the present invention can be appropriately controlled in content range according to requirements such as inhibition of cytokine activity, skin safety, ease of formulation, and the like. In the cosmetic composition or the pharmaceutical composition, the amount of the anti-inflammatory composition to be used is not limited, but may be in the range of 0.001 to 50% by weight, preferably 0.01 to 30.0% by weight, May be included in an amount of 0.01 to 20.0% by weight.

Hereinafter, the cosmetic composition according to one embodiment of the present invention will be described in detail.

The cosmetic composition according to an embodiment of the present invention may be a pharmaceutical composition for anti-inflammation comprising a anti-inflammatory composition comprising glyceryl glucoside and hyaluronic acid as an active ingredient.

In addition, the anti-inflammatory composition further comprises a solvent having two or more hydroxyl groups, thereby providing a cosmetic composition having an improved moisturizing effect along with imparting a fresh feeling of formulation.

For example, when glyceryl glucoside as an active ingredient according to the present invention and glycerin mixed with hyaluronic acid are mixed and used, a gelling phenomenon due to the interaction between glyceryl glucoside and hyaluronic acid in a formulation is induced, and a heavy and slippery hyaluronic acid The feeling of use can be lightly and neatly changed, and at the same time, it can be smoothly applied to the skin to give excellent adhesion.

As another example, glyceryl glucoside as an active ingredient according to the present invention and a mixture of glycerin and hyaluronic acid mixed with at least one selected from 1,2-hexanediol, 1,8-octanediol and 1,10-decanediol In the case of the solvent, it has been confirmed that it can be effectively used as a solubilizing agent which exhibits remarkably improved antimicrobial effect as compared with the use of glyceryl glucoside alone and improves solubility of insoluble or insoluble materials.

The cosmetic composition according to an embodiment of the present invention may be prepared in the form of a general emulsified formulation and a solubilized formulation, etc., by a conventional manufacturing method, in addition to the manufacturing method specifically disclosed in the present invention. The cosmetic composition may be appropriately selected according to the purpose. For example, the cosmetic composition may be selected from the group consisting of softening agents, convergent lotion, nutritional lotion, eye cream, nutritional cream, massage cream, cleansing cream, cleansing foam, cleansing water, And may be formulated into a formulation selected from the group consisting of flavor, essence, pack, and the like, but is not limited thereto.

For example, when the cosmetic composition according to an embodiment of the present invention is an emulsified formulation, the emulsifier, the thickening agent, the emulsion, the oil, the wax, the lubricant, the alcohol, the water-soluble polymer, the gelling agent, , And the like can be used.

As another example, when the cosmetic composition according to one embodiment of the present invention is a solubilized formulation, one or more selected from solvents, solubilizing agents and emulsifying agents may be used as the carrier component. Non-limiting examples of such carrier components include water; C ₁ -C ₄ alcohols; Propylene glycol, and 1,3-butyl glycol; Glycerol aliphatic esters; Water-soluble polypeptides; A water-soluble polymer selected from polyethylene glycol and derivatives thereof; Fatty acid esters of sorbitan selected from Tween 20, Tween 60, Tween 80 and the like; But is not limited thereto.

The cosmetic composition according to an embodiment of the present invention may contain 0.001 to 50% by weight, preferably 0.01 to 30.0% by weight, of the anti-inflammatory composition comprising glyceryl glucoside and hyaluronic acid as an active ingredient, %, More preferably 0.01 to 20.0% by weight.

In addition, the cosmetic composition according to an embodiment of the present invention may further include components included in a functional additive and a general cosmetic composition. Examples of the functional additives include water-soluble vitamins, oil-soluble vitamins, polypeptides, polysaccharides, sphingolipids, ceramide, and seaweed extract; And anti-inflammatory agents, NO inhibitors or COX-2 inhibitors, and the like; But is not limited thereto.

The components contained in the general cosmetic composition may be selected from the group consisting of a preservative, a moisturizer, an emollient, a surfactant, an organic and inorganic pigment, an organic powder, an ultraviolet absorbent, an antiseptic, a bactericide, an antioxidant, a plant extract, Perfumes, blood circulation accelerators, coolants, antiperspirants, purified water, and the like, but are not limited thereto.

Hereinafter, the pharmaceutical composition according to one embodiment of the present invention will be described in detail.

The pharmaceutical composition according to an embodiment of the present invention may be a pharmaceutical composition for preventing and improving inflammatory skin diseases, including a anti-inflammatory composition comprising glyceryl glucoside and hyaluronic acid as an active ingredient.

At this time, the pharmaceutical composition can be directly applied to animals including humans. The animal is a group of organisms corresponding to plants. It mainly consumes organic matter as nutrients, and differentiates digestive organs, excretory or respiratory organs. Preferably, it is a mammal, preferably a human.

The cosmetic composition according to an embodiment of the present invention may contain 0.001 to 50% by weight, preferably 0.01 to 30.0% by weight, of the anti-inflammatory composition comprising glyceryl glucoside and hyaluronic acid as an active ingredient, %, More preferably 0.01 to 20.0% by weight.

The pharmaceutical composition according to an embodiment of the present invention may be formulated into various forms such as oral or parenteral form. The pharmaceutical composition may contain diluents or excipients such as conventional fillers, extenders, binders, wetting agents, disintegrants, surfactants, and the like.

For example, solid preparations for oral administration include tablets, pills, powders, granules, soft or hard capsules, etc. These solid preparations may contain one or more excipients such as starch, calcium carbonate, sucrose (sucrose), lactose, gelatin and the like. In addition to simple excipients, lubricants such as magnesium stearate, talc, and the like are also used. As another example, liquid preparations for oral administration include suspensions, solutions, emulsions, syrups and the like. In addition to water and liquid paraffin which are commonly used simple diluents, various excipients such as wetting agents, sweeteners, And the like.

As another example, formulations for parenteral administration include sterilized aqueous solutions, non-aqueous solvents, suspensions, emulsions, freeze-dried preparations, suppositories, and the like. Examples of the non-aqueous solvent and suspending agent include propylene glycol, polyethylene glycol, vegetable oil such as olive oil, injectable ester such as ethyl oleate, and the like. Examples of the suppository base include witepsol, macrogol, tween 61, cacao paper, laurin, glycerogelatin and the like.

The pharmaceutical composition according to one embodiment of the present invention may be administered parenterally or orally, and may be administered in an amount of 0.01 to 500 mg, preferably 0.1 to 100 mg, per 1 kg of body weight per day, . ≪ / RTI > The dosage for a particular patient may vary depending on the patient's body weight, age, sex, health condition, diet, time of administration, administration method, excretion rate, severity of disease, and the like.

As another example, the external preparation may contain at least one selected from the group consisting of sterilized aqueous solution, non-aqueous solvent, emulsifier, thickener, emulsion, oil, wax, lubricant, alcohol, water-soluble polymer, gelling agent, stabilizer, inorganic powder, One or more selected may be included.

The pharmaceutical composition according to the present invention can be administered orally or parenterally in the form of powders, granules, tablets, soft or hard capsules, oral preparations such as suspensions, emulsions, syrups and sprays, ointments, lotions, creams, gels, And the like, suppositories, injections, sterile injectable solutions, etc., and may be formulated in any form suitable for pharmaceutical preparations. At this time, the pharmaceutical composition in the form of an external preparation such as ointment, lotion, cream, gel, patch, spray, etc. is preferred, but the present invention is not limited thereto.

In addition, the pharmaceutical composition according to an embodiment of the present invention may further comprise a substance used as a known substance having a known anti-inflammatory effect, such as an anti-inflammatory agent, an NO inhibitor or a COX-2 inhibitor, Of course.

The pharmaceutical composition according to one aspect of the present invention has an effect of preventing and improving inflammatory skin diseases. Non-limiting examples of the inflammatory skin disease include atopic dermatitis, psoriasis, contact dermatitis, eczematous dermatitis, dermatitis dermatitis, dermatitis dermatitis, herpes dermatitis, herpes dermatitis, squamous cell carcinoma, gingivosclerosis, pemphigus, , Systemic sclerosis, dermatomyositis, multiple myositis, inflammatory muscle lesion, leprosy or triceps, and particularly excellent effects such as atopic dermatitis, psoriasis, contact dermatitis and the like are excellent.

 Hereinafter, preferred embodiments of the present invention will be described in order to facilitate understanding of the present invention. However, the following examples are provided only for the purpose of easier understanding of the present invention, and the following examples are merely illustrative and not intended to limit the scope of the present invention in any way.

(Confirm cytotoxicity)

Using the compositions prepared in the following Examples and Comparative Examples, the cell viability of human fibroblasts (ATCC 2076) was measured. Human fibroblast (ATCC 2076) was inoculated into a 24-well culture plate of IMDM (Iscove's Modified Dulbecco's Medium, GIBCO) containing 10% bovine serum at a concentration of 5 x 10 ⁴ cells / ml. After 24 hours of inoculation, the medium was replaced with serum-free medium. Then, the test sample was added at a concentration of 1, 10, 100 μg / ml and cultured in a 5% CO ₂ incubator at 37 ° C. for one day. After the incubation, the supernatant was removed and further washed with 200 μl of 5% PBS (phosphate buffered saline). Next, 1.0 ml of MTT solution was added to each well, MTT was removed after 4 hours, 1.0 ml of DMSO was added to each well, and the mixture was incubated at 37 ° C for 15 hours. Thereafter, the absorbance at 570 nm was measured, and the cell viability was determined using the following formula (1). The results are shown in Table 2 below. At this time, as the negative control group, an untreated control group without the active ingredient was employed.

(Equation 1)

Cell survival rate (%) = (A _{570? Value} / B _{570? Value} ) × 100

A: absorbance value at 570 nm of the example

B: absorbance value at 570 nm of negative control group

(Evaluation of anti-inflammatory activity)

The compositions prepared in the following examples and comparative examples were used to evaluate IL-8, MCP-1 and IL-6 inhibitory activity by LPS stimulation in macrophage cells. Human macrophage cell line THP-1 cells (KCLB, 40202) were seeded at ⁶ × 10 ⁶ cells / well in a 6-well plate and cultured in a cell incubator for 12 hours.

Then, the final concentration of the anti-inflammatory composition prepared in Example 1 was adjusted to 1, 10, and 100 / / ml, respectively. After 21 hours, the final concentration of LPS was further adjusted to 20 / / Lt; / RTI > (IL-8), monocyte chemoattractant protein-1 (MCP-1), interleukin-6 (IL-6) ELISA kit (Inhibitory effect) of IL-8, MCP-1, and IL-6 by LPS was measured using a commercially available anti-inflammatory agent (BD pharmigen, USA)

The inhibitory activity was determined by plotting standard curves based on the respective absorbances of the recombinant IL-8, MCP-1 and IL-6, which are standard substances, to calculate the reaction equation between the absorbance and the standard substance, Secretion of interleukin-8 or monocyte chemoattractant protein-1 was obtained. Then, the stimulation relaxation rate was evaluated by the following equation (1).

(Equation 1)

IL-8, MCP-1 or IL-6 in the treated group / IL-8, MCP-1 or IL-6 increased in the treated group / 100% Increased secretion)]

(Evaluation of antibacterial activity)

Staphylococcus aureus ATCC 6538P as a gram-positive bacterium, Escherichia coli ATCC 8739 as a gram-negative bacterium, Pseudomonas aeruginosa ATCC 8738 as a gram-positive bacterium for measuring the antimicrobial activity of the compositions prepared in the following Examples and Comparative Examples, 9027), Candida albicans ATCC 10231 and Aspergillus niger ATCC 22343 were used as yeast.

Approximately 50 μl of each of the cultivated strains was added to a solidified plate medium, and the mixture was dispensed into a plate culture medium and uniformly smoothed using a spreader. About 40 μl of each composition was absorbed into a paper disk having a diameter of 10 mm, the solvent was dried, the microorganism was closely adhered to the surface of the medium on which the strain had been coated, and cultured in an incubator at 30 ° C. for more than 48 hours. And the size of the clear zone formed in the test piece was measured to confirm the antibacterial effect. Since microorganisms can not grow near the paper disk, the larger the average diameter value, the better the antimicrobial activity. In addition, methylparaben (MP) was used as a positive control, and the same procedure was followed. At this time, the greater the diameter, the higher the antibacterial effect of the strain. The results are shown in Table 4 below.

(Example 1-5)

After preparing the anti-inflammatory composition according to the composition shown in the following Table 1, cytotoxicity and anti-inflammation / antibacterial effect were evaluated by the above-mentioned method.

(Comparative Example 1-6)

After preparing the composition with the composition shown in the following Table 1, cytotoxicity and anti-inflammation / antibacterial effect were evaluated by the above-mentioned method.

(-) - catechin was found to precipitate within 1 day after emulsification in the case of the compositions prepared in the composition of Table 1, and in Comparative Examples 4 to 6, especially in Comparative Examples 4 and 5 The stability was poor.

As shown in Table 2, the cell survival rate of the anti-inflammatory composition according to the present invention was not substantially reduced as compared with the control. This means that the anti-inflammatory composition according to the present invention does not show toxicity to the cells at the test concentration. Furthermore, it was found that when the specific ratio according to the present invention is satisfied, it is excellent in cytotoxicity.

As shown in Table 3, the anti-inflammatory composition according to the present invention effectively inhibits inflammation-related cytokines (such as IL-6) and chemokines (such as IL-8 and MCP-1) By inhibiting NO formation secreted from macrophages, it has an excellent anti-inflammatory effect.

In particular, inhibition of IL-6 expression was inhibited by at most 220%, inhibition of MCP-1 expression was inhibited by at least 197%, and inhibition of IL-8 expression was inhibited by the inhibition of IL-6 expression in comparison with Comparative Examples 1 and 2 in which glyceryl glucoside or hyaluronic acid alone was used It is confirmed that the anti-inflammatory effect remarkably improved to at most 410% (Comparative Example 2 100 μg / ml vs Example 4 100 μg / ml). In addition, the anti-inflammatory composition according to the present invention suppresses the secretion of IL-8, MCP-1 and IL-6 in a concentration-dependent manner, and especially when the concentration is 100 μg / ml, there was.

In addition, the anti-inflammatory composition according to the present invention improves the solubilization ability of polyphenols (e.g., catechins, quercetin, etc.) having a very low solubility in water or insoluble therein, Respectively.

As shown in Table 4, it was found that the anti-inflammatory composition according to the present invention exhibits remarkably improved synergistic effect in antibacterial effect as well as excellent anti-inflammatory effect. The above-mentioned effect on antibacterial is based on methylparaben known as synthetic antimicrobial agent.

According to the present invention, it is possible to provide a anti-inflammatory composition that does not cause skin side effects and can effectively inhibit skin inflammation. In addition, according to the present invention, it is possible to impart an ideal pharmacological action, an effect and an effect to the prevention and improvement of an inflammatory skin disease by the excellent adhesion to the skin, and it can be formulated into various forms as a new anti- do.

(Formulation Example 1)

Lotions were prepared according to a conventional method with the compositions shown in Table 5 below.

(Formulation Example 2)

Nutrition cream was prepared according to a conventional method with the composition shown in Table 6 below.

(Formulation Example 3)

Ointment was prepared according to a conventional method with the composition shown in Table 7 below.

(Formulation Example 4)

A gel was prepared according to a conventional method with the composition shown in Table 8 below.

While the present invention has been particularly shown and described with reference to exemplary embodiments thereof, it is to be understood that the technical scope of the present invention is not limited to the disclosed exemplary embodiments. Accordingly, the actual scope of the present invention will be defined by the appended claims and their equivalents.

Claims (12)

Glyceryl glucoside and hyaluronic acid as an active ingredient. The method according to claim 1,
Further comprising a solvent having two or more hydroxyl groups. 3. The method of claim 2,
The solvent having a hydroxyl group is selected from glycerin, 1,3-propanediol, 1,3-butanediol, 1,5-pentanediol, 1,2-hexanediol, 1,8-octanediol and 1,10- Lt; / RTI > 3. The method of claim 2,
≪ / RTI > further comprising a flavonoid. 5. The method of claim 4,
Wherein the flavonoid is selected from the group consisting of apigenin, catechin, daidzein, genistein, camperol, naringinin, quercetin, and derivatives thereof. The method according to claim 1,
Wherein the glyceryl glucoside and hyaluronic acid are mixed in a weight ratio of 1: 0.1 to 1: 2. The method according to claim 1,
Wherein said anti-inflammatory composition is involved in the inhibition of at least one of the expression of interleukin-6, the expression of interleukin-8, and the expression of monocyte chemoattractant protein-1. The method according to claim 1,
Wherein the anti-inflammatory composition is a pharmaceutical composition or a cosmetic composition. 9. The method of claim 8,
Wherein the cosmetic composition is formulated into a softening agent, a convergent lotion, a nutritional lotion, an eye cream, a nutritional cream, a massage cream, a cleansing cream, a cleansing foam, a cleansing water, a powder, an essence or a pack. 9. The method of claim 8,
Wherein the pharmaceutical composition is formulated into a lotion, ointment, gel, cream, patch or spray. 9. The method of claim 8,
The pharmaceutical composition is useful as an anti-inflammatory agent for the prevention and / or amelioration of inflammatory skin diseases. 12. The method of claim 11,
The inflammatory skin disease is selected from the group consisting of atopic dermatitis, psoriasis, contact dermatitis, eczematous dermatitis, dermatitis dermatitis, dermatitis dermatitis, herpes dermatitis, herpes zoster dermatitis, squamous cellulitis, scleroderma, gangrenous epidermolysis, , Multiple myositis, inflammatory muscle lesions, leprosy or triceps.